Pharmacokinetics of multiple dose antofloxacin hydrochloride in Chinese healthy subjects
10.13699/j.cnki.1001-6821.2017.13.014
- VernacularTitle:盐酸安妥沙星片在健康受试者多剂给药的药代动力学
- Author:
Cai-Yun ZHAO
1
;
Min-Ji WEI
;
Yuan L(U)
;
Xiang-Yan LI
;
Rui-Rui HE
;
Tian-Yun LI
;
Yan LIU
;
Ya-Hong XIA
;
Ji-Hong TIAN
;
Yan MA
Author Information
1. 北京大学第一医院临床药理研究所
- Keywords:
antofloxacin;
pharmacokinetic;
fast;
food;
HPLC
- From:
The Chinese Journal of Clinical Pharmacology
2017;33(13):1216-1220
- CountryChina
- Language:Chinese
-
Abstract:
Objective To evaluate the pharmacokinetics of multiple dose of antofloxacin hydroehloride tablet under fast and food state in Chinese healthy subjects.Methods A randomized,open and multiple dose study was conducted.Three dose groups with 16 subjects per group were given the dose of 200,400 and 600 mg antofloxacin hydrochloride tablet,once daily for 7 days respectively.8 subjects (4 male and 4 female) were administrated under fast state and 8 subjects (4 male and 4 female) under food state in each dose.The concentrations of antofloxacin in plasma and urine were determined by HPLC method.Results The main pharmacokinetics parameters of three dose (200,400 and 600 mg) under fast at first day were as follows:Cmax were (2.23 ±0.38),(4.59 ± 1.40),(5.03 ±0.77)mg · L-1,t1/2βwere(11.99 ±3.31),(10.97 ±5.33),(14.39 ± 1.63)h,tmax were (1.37 ±0.78),(2.04 ± 1.42),(2.90 ±2.02)h,AUC0-t were (27.61 ±6.14),(51.77 ±22.09),(73.62 ±10.14)mg · L-1 · h,AUC0-∞ were (38.28 ± 13.49),(72.28 ± 42.80),(108.91 ± 13.26) mg · L-1 · h,V/F were (92.84 ± 12.98),(91.90±14.55),(116.28±22.62)L,CL/F were (5.73 ±1.71),(7.67 ±4.65),(5.58 ±0.66)L· h-1,respectively;under food state at first day,Cmax were (2.36 ± 0.43),(4.11 ± 1.53),(5.60 ± 1.00) mg · L-1,t1/2β were (14.37 ±4.34),(11.25 ±5.39),(15.53 ±2.94) h,tmax were (2.69 ± 1.62),(2.40 ± 1.50),(2.65 ±1.29)h,AUC0-t were (33.69 ±4.00),(48.07 ±22.19),(78.01 ±17.18)mg · L-1 · h,AUC0-∞ were (50.71 ± 8.86),(67.37 ± 41.98),(121.31.66 ± 33.54) mg · L-1 · h,V/F were (81.04 ± 16.35),(106.32 ±34.33),(114.08±20.00)L,CL/Fwere (4.07 ±0.82),(8.28 ±5.29),(5.23 ±1.18)L · h-1,respectively.After 7 days,the main pharmacokinetics parameters of three dose (200,400 and 600 mg) under fast were as follows:Cmax were (3.69 ± 1.39),(7.54 ± 2.95),(8.50 ± 0.93) mg · L-1,t1/2β were (25.22 ± 3.34),(19.56 ±12.47),(15.95 ±2.85)h,tmax were (1.64±1.29),(1.31 ±0.79),(1.60±1.07)h;AUC0-twere (72.29 ± 24.00),(142.96 ± 67.20),(180.81 ± 35.33) mg · L-1 · h,AUC0-∞ were (75.90 ± 25.46),(148.26 ±69.86),(183.30±35.11)mg · L-1 · h,V/F were (184.77 ±52.51),(119.22 ±53.92),(118.91 ±30.13) L,CL/F were (5.06 ± 1.18),(4.75 ± 1.72),(5.15 ±0.72)L · h-1;under food state,Cmax were (3.53 ± 1.06),(6.54 ±1.43),(8.52 ±1.80)mg · L-1,t1/2βwere (24.08 ±6.12),(20.64 ±9.16),(18.69 ±6.49)h,tmax were (2.94 ± 1.02),(1.96 ± 1.05),(2.69 ±0.96)h,AUC0-t were (94.71 ±31.03),(142.17 ±52.46),(211.34.01 ±52.99)mg · L-1 · h,AUC0-∞were (99.32 ±33.93),(149.77 ±55.19),(213.76 ±53.00)mg· L-1 · h,V/F were (139.40±37.39),(140.24±71.11),(130.20 ±71.09)L;CL/F were (4.11 ±1.13),(4.81 ± 1.17),(4.69 ± 0.88)L · h-1.Urinary recovery rates after 7 days doses from zero to 120 h were (67.24±13.56)％,(68.62±14.45)％ and (74.31 ±12.99)％,respectively.Conclusion Food had no obvious influence on pharmacokinetics parameters after multiple oral dose of 200,400 and 600 mg antofloxacin hydrochloride tablet under fast and food state,except that tmax increased.There was no accumulation in human body.It can be considered that food had no effect in the clinical use of antofloxacin hydrochloride tablet.
